Objective:To establish the content determination method for astragaloside in Bushen Wenfei mixtures by HPLC-ELSD. Methods:HPLCwithanAgilentZORBAXC18(150mm×4.6mm,5μm)columnwasused. Methanol-water(75∶25)wasusedasthe mobile phase and the flow rate was 0. 8 ml·min-1 . The drift tube temperature was 80℃ and the gas flow rate was 2. 5 ml·min-1 . Results: The linear range of astragaloside was 0.297-4.944 μg (r =0.999 7). The average recovery was 98.13% with RSD of 1. 27%(n=9). Conclusion:The method is with sufficient accuracy, stability and repeatability, and can be used in determination of Bushen Wenfei mixtures.

Objective To investigate the effect of prehospital transport mode on delay care in patients withacutestroke.Methods From March 2016 to August 2016,a total of 255 consecutive patients with acute stroke who met the inclusion criteria in Xuanwu Hospital,Capital Medical University were analyzed prospectively. Seven patients were excluded because of incomplete data. A total of 248 valid cases were enrolled. They were divided into either an ambulance transport group (n=88)or a non-ambulance transport group (n=160)according to whether they were transported by ambulance or not. The differences of the baseline data,prehospital status,onset-to-door time,door-to-examination time,door-to-CT scan time,door-to-intravenous thrombolysis time of the 2 groups were compared,and the related factors of ambulance use were analyzed in patients with acute stroke. Results (1)The ambulance utilization rate of 248 patients was 35. 5%. The age,the coronary heart disease rate,National Institutes of Health Stroke Scale (NIHSS)score of the patients in the ambulance transport group were higher than those of the non-ambulance transport group. There were significant differences between the two groups (65 ± 11 vs. 61 ± 11 years,15. 9%[14/88]vs. 5. 6%[9/160],9 [3,17]vs. 2 [1,5];all P <0. 05). The stroke rate of the patients in the ambulance transport group was lower than that of the non-ambulance transport group(23. 9%[21/88]vs. 37. 5%[60/160],P<0. 05). (2)There were significant differences in self-identified acute disease and self-health care consciousness between the ambulance transport group and the non-ambulance transport group (all P<0. 01). (3)Compared with the non-ambulance transport group,the onset-to-door time,door-to-examination time,door-to-CT scan time,door-to-intravenous thrombolysis time were shorter in patients of the ambulance transport group (102[64,150]min vs. 136[86,230]min,3[1,8]min vs. 7[4,11]min, 15[18,23]min vs. 16[22,27]min,and 41 ± 9 min vs. 50 ± 10 min;all P <0. 05). (4)The result of Logistic regression analysis showed that the acute stroke patients with advanced age (OR,1. 04,95%CI 1. 01-1. 08,P =0. 01),higher NIHSS score (OR,1. 13,95%CI 1. 08-1. 19,P <0. 01),they or the insiders thought that the disease was emergent (OR,17. 08,95%CI 5. 78-50. 41,P<0. 01),they would seek medical advice in time when they felt sick (OR,38. 13,95%CI 10. 13-143. 61,P<0. 01),and they would take medicine by themselves when they felt sick (OR,6. 82,95%CI 2. 33-19. 99,P<0. 01)were more likely to be transported to hospital by ambulance.Conclusion Using ambulance can reduce the treatment de-lay for patients with acute stroke. The patients with self-health care consciousness are more likely to choose am-bulance transport. The importance of using ambulance should be strengthened for patients with stroke.

Objective To analyze the efficacy and safety of hypofractionated stereotactic radiotherapy ( FSRT ) combined with temozolomide ( TMZ ) for large brain metastases ( BMs ) in a prospective phaseⅡclinical trial.Methods From 2010 to 2015, a total of 33 patients were enrolled as subjects.The median Karnofsky Performance Status scores before and after treatment were 70 and 80, respectively.The major primary tumor was non-small cell lung cancer (57.6%).The brain metastasis had a diameter of≥3 cm or a volume of ≥6 cm3 .The radiation dose was 52 Gy in 13 fractions or 52.2 Gy in 15 fractions.Patients received TMZ at a dose of 75 mg/m2 per day concurrently.The radiotherapy was followed by 6 cycles of adjuvant treatment with TMZ (150 mg/m2, days 1-5, 28 days per cycle).Patients were reexamined by magnetic resonance imaging ( MRI) during the treatment.The radiation field would be shrunk if the gross target volume ( GTV) was reduced by≥20%.The treatment outcomes were evaluated by MRI at 2-3 months after treatment.Results The total numbers of tumors and GTVs were 95 and 38, respectively. Twenty-four (63%) out of the 38 GTVs had a volume larger than 10 cm3 and the median GTV was 15.3 cm3 (5.7-142.8 cm3).Twenty-two (67%) out of the 33 patients achieved field shrinking during the treatment, and the median reduction rate of GTV was 44%( 21%-88%) .The median total dose was 59.5 Gy, and 100%and 21.2%of patients completed the concurrent and adjuvant treatment with TMZ, respectively.In all patients, the overall response rate was 97.0%;the 1-year local control, intracranial progression-free
survival, and overall survival rates were 97%, 70%, and 62%, respectively;the median survival time was 15.3 months.The main adverse reactions were grade 1-2 nausea and vomiting.One patient got grade 3 liver function impairment.Conclusions FSRT combined with TMZ is a safe and effective approach for treating large BMs.More than 50%of patients can achieve field shrinking to shorten treatment duration and reduce toxicity.Clinical Trial Registry ClinicalTrials.gov,registration number:NCT02654106.

OBJECTIVE:To observe the effects of insulin glargine in type 2 diabetes mellitus patients with poor glucose con-trol by rosiglitazone and metformin. METHODS:A total of 90 patients with type 2 diabetes mellitus with poor glucose control by rosiglitazone and metformin admitted to our hospital from Aug. 2013 to Dec. 2015 were divided into control group and observation group according to random number table,with 45 cases in each group. Control group was given Acarbose tablets 50 mg orally be-fore meal,tid,with maximal dose of 300 mg/d. Observation group was given Insulin glargine injection subcutaneously,qd,with initial dose of 0.15 u/kg,adjusted according to blood glucose monitoring,with maximal dose of 40 u/d. Both group were treated for 24 weeks. The levels of fasting blood glucose,2 h postprandial blood glucose,HbA1c,fasting C peptide and 2 h postprandial C peptide were compared between 2 groups before and after treatment. The time of blood glucose reaching target and the occur-rence of adverse events were recorded,and the incidence of adverse events was calculated. RESULTS:Before treatment,there was no statistical significance in above indexes between 2 groups(P>0.05). After treatment,The levels of fasting blood glucose and 2 h postprandial blood glucose in 2 groups were significantly lower than before treatment,and the levels of fasting C peptide,2 h postprandial C peptide and HbA1c were significantly higher than before treatment;except for fasting blood glucose,above indexes of observation group were significantly better than those of control group,with statistical significance (P<0.05). The time of blood glucose reaching target in observation group was significantly shorter than control group,the incidence of nocturnal hypogly-cemia,severe hypoglycemia,edema and gastrointestinal reactions and total adverse events in observation group were significantly lower than control group,with statistical significance(P<0.05). CONCLUSIONS:The application of insulin glargine in type 2 di-abetes mellitus patients with poor glucose control by rosiglitazone and metformin can effectively reduce the levels of blood glucose and HbA1c,and improve islet function with good safety.

This study is to investigate the chemical constituents from the whole plant Corydalis edulis. The chemical constituents were separated and purified by macroporous resin D101, silica gel, Sephadex LH-20, ODS, and semi-preparative HPLC. Their structures were determined by physicochemical properties and spectroscopic data. Four compounds were isolated from the dichloromethane and water extracts of the whole plant C. edulis, and identified as 6'-β-D-xylosylicariside B2(1),(3S,5R,6S,7E)-5,6-epoxy-3-hydroxy-7-megastigmen-9-one(2), loliolide(3), and 5,5'-dimethoxybiphenyl-2,2'-diol(4), respectively. Compound 1 is a new compound, of which the absolute configuration was established by electronic circular dichroism(ECD) calculations. Compound 4 is obtained from the plants of Papaveraceae family for the first time. Compounds 2 and 3 are firstly isolated from the Corydalis genus.
Chromatography, High Pressure Liquid ; Corydalis/chemistry* ; Glycosides/isolation & purification* ; Molecular Structure ; Phytochemicals/isolation & purification* ; Sesquiterpenes/isolation & purification*

To synthesize a series of 3-, 4-, and/or 11-trihydroxy modified bergenin derivatives and evaluated their cytotoxic activity in vitro. The phenolic hydroxyl groups of bergenin were protected by benzyl groups with benzyl bromide. Treatment of dibenzyl bergenin with the corresponding acid in the presence of EDC·HCl and DMAP in CH2Cl2, followed by hydrogenation over Pd/C catalysts, afforded derivatives of bergenin esters. All of the target compounds were identified by IR, MS, and (1)H NMR. Twenty-six novel and three known derivatives of bergenin esters were synthesized. Their cytotoxicity values were evaluated by the MTT assay on the inhibition of DU-145 and BGC-823 cells in vitro. Several triply-substituted (3a, 4a, 5a, 6a, 7a) and doubly-substituted (8b, 9b) bergenin derivatives exhibited higher cytotoxic activity than bergenin. The result showed that the size of substituents and the lipophilicity of the bergenin esters displayed an important role on their cytotoxic activity.
Antineoplastic Agents, Phytogenic ; chemical synthesis ; pharmacology ; therapeutic use ; Benzopyrans ; pharmacology ; therapeutic use ; Cell Line, Tumor ; Dipterocarpaceae ; chemistry ; Humans ; Male ; Molecular Structure ; Phytotherapy ; Plant Extracts ; pharmacology ; therapeutic use ; Prostatic Neoplasms ; drug therapy ; Stomach Neoplasms ; drug therapy ; Structure-Activity Relationship

OBJECTIVE: To explore the anti-inflammatory effects of ethyl lithospermate in lipopolysaccharide (LPS)-stimulated RAW 264.7 murine-derived macrophages and zebrafish, and its underlying mechanisms. METHODS: 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazoliumbromide (MTT) assays were performed to investigate the toxicity of ethyl lithospermate at different concentrations (12.5-100 µ mol/L) in RAW 264.7 cells. The cells were stimulated with LPS (100 ng/mL) for 12 h to establish an inflammation model in vitro, the production of pro-inflammatory cytokines interleukin (IL)-6 and tumor necrosis factor α (TNF-α) were assessed by enzyme linked immunosorbent assay (ELISA). Western blot was used to ascertain the protein expressions of signal transducer and activator of transcription 3 (STAT3), nuclear factor kappa B (NF-κB) p65, phospho-STAT3 (p-STAT3, Tyr705), inhibitor of NF-κB (IκB) α, and phospho-I κB α (p-IκB α, Ser32), and confocal imaging was used to identify the nuclear translocation of NF-κB p65 and p-STAT3 (Tyr705). Additionally, the yolk sacs of zebrafish (3 days post fertilization) were injected with 2 nL LPS (0.5 mg/mL) to induce an inflammation model in vivo. Survival analysis, hematoxylin-eosin (HE) staining, observation of neutrophil migration, and quantitative real-time polymerase chain reaction (qRT-PCR) were used to further study the anti-inflammatory effects of ethyl lithospermate and its probable mechanisms in vivo. RESULTS: The non-toxic concentrations of ethyl lithospermate have been found to range from 12.5 to 100 µ mol/L. Ethyl lithospermate inhibited the release of IL-6 and TNF-α(P<0.05 or P<0.01), decreased IκBα degradation and phosphorylation (P<0.05) as well as the nuclear translocation of NF-κB p65 and p-STAT3 (Tyr705) in LPS-induced RAW 264.7 cells (P<0.01). Ethyl lithospermate also decreased inflammatory cells infiltration and neutrophil migration while increasing the survival rate of LPS-stimulated zebrafish (P<0.05 or P<0.01). In addition, ethyl lithospermate also inhibited the mRNA expression levels of of IL-6, TNF-α, IκBα, STAT3, and NF-κB in LPS-stimulated zebrafish (P<0.01). CONCLUSION Ethyl lithospermate exerts anti-Inflammatory effected by inhibiting the NF-κB and STAT3 signal pathways in RAW 264.7 macrophages and zebrafish.
Animals ; Mice ; NF-kappa B/metabolism* ; Lipopolysaccharides ; RAW 264.7 Cells ; Zebrafish ; NF-KappaB Inhibitor alpha/metabolism* ; Interleukin-6/metabolism* ; Tumor Necrosis Factor-alpha/metabolism* ; STAT3 Transcription Factor/metabolism* ; Inflammation/metabolism* ; Anti-Inflammatory Agents/therapeutic use*

Two new phenylpropanoid amide glycosides and ten analogues were isolated from the CH_2Cl_2 layer of 95% ethanol extract of the whole plants of Corydalis racemosa by using various chromatographic techniques, including silica gel, Sephadex LH-20, ODS column chromatographies, and semi-preparative HPLC. Their structures were identified on the basis of physicochemical properties, MS, NMR, and IR spectroscopic data as N-cis-sinapoyltyramine-4'-O-β-glucoside(1), N-cis-sinapoyl-3-methoxytyramine-4'-O-β-glucoside(2), N-cis-sinapoyltyramine(3), N-cis-feruloyltyramine(4), N-trans-cinnamoyltyramine(5), N-trans-feruloylphenethylamine(6), N-trans-p-methoxycinnamoyl-3-hydoxyoctopamine(7), N-cis-feruloyl-3-methoxytyramine(8), N-trans-feruloyltyramine(9), N-trans-feruloyl-3-methoxytyramine(10), N-trans-sinapoyltyramine(11), and N-trans-p-coumaroyltyramine(12). Compounds 1 and 2 are new compounds. Compounds 3-7 are obtained from the plants of Papaveraceae for the first time, and compounds 8-12 are firstly isolated from C. racemosa.
Amides ; Chromatography, High Pressure Liquid ; Corydalis ; Glucosides ; Glycosides

Overactive bladder (OAB) is the most bothersome symptom in lower urinary tract symptoms (LUTS). Current pharmacologic treatment aims to inhibit detrusor contraction; however, shows unsatisfied efficacy and high discontinuation rate. LIM kinases (LIMKs) promote smooth muscle contraction in the prostate; however, their function in the bladder smooth muscle remains unclear. Here, we studied effects of the LIMK inhibitors on bladder smooth muscle contraction and proliferation both